HETEROCYCLIC COMPOUNDS AND USE THEREOF IN TREATING OR PREVENTING BACTERIAL INFECTIONS Russian patent published in 2021 - IPC C07D471/08 C07D513/04 A61K31/439 A61K31/444 A61K31/497 A61K31/501 A61K31/506 A61K31/513 A61K31/546 A61P31/04 

Abstract RU 2741496 C2

FIELD: pharmaceuticals.

SUBSTANCE: invention relates to a compound selected from a group consisting of a compound having formula (I), in which R1 is A and R2 is B, and a compound having formula (I), where R1 is B and R2 is A, where A is unsubstituted or substituted with one or two substitutes T1, a saturated or aromatic 4–6, 9-member heterocycle, where 4–6, 9-member heterocycle is 5- or 6-member monocyclic heterocycle containing one nitrogen atom and further containing one or two additional heteroatoms, selected from O, S and N, or 4- or 6-member monocyclic heterocycle containing one nitrogen atom; or 9-membered bicyclic heterocycle, containing at least one nitrogen atom and additionally containing one, two or three additional heteroatoms or a heteroatomic group selected from S and N; B is a hydrogen atom; or unsubstituted (C1-C3)-alkyl; R3 is -SO3H or -CF2COOH; Q1 and Q2, identical or different, independently represent a hydrogen atom; -(CH2)r-NHQ3; -(CH2)r-OQ3; -(CH2)n-CONHQ3; or unsubstituted (C1-C3)-alkyl; aromatic 5-member heterocycle containing one nitrogen atom and one oxygen atom; Q3 represents a hydrogen atom; T1, identical or different, independently represent a fluorine atom; -(CH2)mOQ1; -(CH2)m-CN; -(CH2)m-C(O)OQ1; -(CH2)m-C(O)NQ1Q2; -(CH2)m-C(O)NQ1OQ2; -(CH2)m-NQ1Q2; -(CH2)m-NH-C(NHQ3)=NQ4; or T1, identical or different, independently represent unsubstituted 5-member aromatic heterocycle containing one nitrogen atom and further containing one additional heteroatom, selected from S; (C1-C3)-alkyl; m, identical or different, are independently equal to 0, 1, 2; r is equal to 1, 2; any carbon atom in the group selected from the heterocycle can be oxidised to form a C=O group. Invention also relates to pharmaceutical compositions, to use of compound or composition, to compound.

(I)

EFFECT: obtaining novel compounds of formula (I) which can be used to prevent or treat bacterial infection caused by gram-negative bacteria.

10 cl, 4 tbl, 51 ex

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RU 2 741 496 C2

Authors

Oliveira, Chrystelle

Le Fralliec, Geraldine

Faivre, Fabien

Briet, Sophia

Brias, Julie

Vomscheid, Sophie

Simon, Christophe

Richard, Sebastien

Le Strat, Frederic

Ledoussal, Benoit

Lecointe, Nicolas

Chevreuil, Francis

Chasset, Sophie

Caravano, Audrey

Barbion, Julien

Dates

2021-01-26Published

2016-05-06Filed